Ontology highlight
ABSTRACT:
SUBMITTER: Rai G
PROVIDER: S-EPMC4033661 | biostudies-literature | 2014 May
REPOSITORIES: biostudies-literature
Rai Ganesha G Joshi Netra N Jung Joo Eun JE Liu Yu Y Schultz Lena L Yasgar Adam A Perry Steve S Diaz Giovanni G Zhang Qiangli Q Kenyon Victor V Jadhav Ajit A Simeonov Anton A Lo Eng H EH van Leyen Klaus K Maloney David J DJ Holman Theodore R TR
Journal of medicinal chemistry 20140513 10
A key challenge facing drug discovery today is variability of the drug target between species, such as with 12/15-lipoxygenase (12/15-LOX), which contributes to ischemic brain injury, but its human and rodent isozymes have different inhibitor specificities. In the current work, we have utilized a quantitative high-throughput (qHTS) screen to identify compound 1 (ML351), a novel chemotype for 12/15-LOX inhibition that has nanomolar potency (IC50 = 200 nM) against human 12/15-LOX and is protective ...[more]